GSK973


Catalog No. Size PriceQuantity
M30128-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).

Product information

CAS Number: 2138473-38-6

Molecular Weight: 410.44

Formula: C23H23FN2O4

Chemical Name: (2S,3S)-2-(fluoromethyl)-N7-methyl-N5-[(1R,5S)-3-oxabicyclo[3.1.0]hexan-6-yl]-3-phenyl-2,3-dihydro-1-benzofuran-5,7-dicarboxamide

Smiles: CNC(=O)C1=CC(=CC2[C@@H]([C@@H](CF)OC=21)C1=CC=CC=C1)C(=O)NC1[C@H]2COC[C@H]21

InChiKey: WZQLVEPIBAOOGF-SFDMMAKQSA-N

InChi: InChI=1S/C23H23FN2O4/c1-25-23(28)15-8-13(22(27)26-20-16-10-29-11-17(16)20)7-14-19(12-5-3-2-4-6-12)18(9-24)30-21(14)15/h2-8,16-20H,9-11H2,1H3,(H,25,28)(H,26,27)/t16-,17+,18-,19+,20?/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

GSK973 (1 mg/kg; i.v.) treatment shows the CL, CIrenal, Vss, and T1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively. GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%.

Products are for research use only. Not for human use.

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